- NEW COMPOUND AND USE THEREOF
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PROBLEM TO BE SOLVED: To provide a compound for visualizing TRPA1 in an organism. SOLUTION: The invention provides a compound represented by the formula (1) or (2) in the figure or a salt thereof. (In the formulas, R1 and R2 are each a substituent having a radioisotope.) SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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- Discovery, optimization, and biological evaluation of 5-(2- (trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists
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A high throughput screening campaign identified 5-(2-chlorophenyl)indazole compound 4 as an antagonist of the transient receptor potential A1 (TRPA1) ion channel with IC50 = 1.23 μM. Hit to lead medicinal chemistry optimization established the SAR around the indazole ring system, demonstrating that a trifluoromethyl group at the 2-position of the phenyl ring in combination with various substituents at the 6-position of the indazole ring greatly contributed to improvements in vitro activity. Further lead optimization resulted in the identification of compound 31, a potent and selective antagonist of TRPA1 in vitro (IC50 = 0.015 μM), which has moderate oral bioavailability in rodents and demonstrates robust activity in vivo in several rodent models of inflammatory pain.
- Rooney, Lisa,Vidal, Agnès,D'Souza, Anne-Marie,Devereux, Nick,Masick, Brian,Boissel, Valerie,West, Ryan,Head, Victoria,Stringer, Rowan,Lao, Jianmin,Petrus, Matt J.,Patapoutian, Ardem,Nash, Mark,Stoakley, Natalie,Panesar, Moh,Verkuyl, J. Martin,Schumacher, Andrew M.,Petrassi, H. Michael,Tully, David C.
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p. 5129 - 5140
(2014/07/08)
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- TETRACYCLIC COMPOUND
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Provided are a tetracyclic compound represented by the formula (I): [in the formula(I),the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents -O- or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, 1, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.
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Page/Page column 47
(2011/04/25)
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- Arylindazoles and their use as herbicides
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This invention relates to substituted aryl indazoles, a process for producing them and their use as herbicides. In particular this invention relates to substituted aryl indazoles of the formula STR1 wherein all variables are as defined in the specification.
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